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4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)-

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4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Suppliers list
Company Name: TargetMol Chemicals Inc.
Tel: +1-781-999-5354
Email: support@targetmol.com
Products Intro: Product Name:ARN-21934
CAS:2230854-93-8
Package:1 mg；1 mL * 10mM (in DMSO)；10 mg；100 mg；25 mg；5 mg；50 mg Remarks:REAGENT;FOR LABORATORY USE ONLY
Company Name: Wuhan Topule Biopharmaceutical Co., Ltd
Tel: +8618327326525
Email: masar@topule.com
Products Intro: Product Name:ARN-21934
CAS:2230854-93-8
Purity:98% Package:100mg;1g;500g Remarks:Topule Company operates with integrity and has its own laboratory, which supports packaging and customization. Payment will be made after the product has passed third-party testing
Company Name: Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd
Tel: +86-18341751992 +86-15382112998
Email: 757984502@qq.com
Products Intro: Product Name:ARN-21934
CAS:2230854-93-8
Purity:0.98 Package:100mg;500mg;1g;5g Remarks:existing product
Company Name: Aladdin Scientific
Tel: +1-+1(833)-552-7181
Email: sales@aladdinsci.com
Products Intro: Product Name:ARN-21934
CAS:2230854-93-8
Purity:98% Package:$350.9/5mg;$580.9/10mg;$1100.9/25mg;$1700.9/50mg;$2500.9/100mg;Bulk package Remarks:98%
Company Name: Wuhan Jingkang en Biomedical Technology Co., Ltd
Tel: +8613720134139
Email: orders@jknbiochem.com
Products Intro: Product Name:ARN-21934
CAS:2230854-93-8
Purity:0.98 Package:10G:100G
4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Basic information
Product Name:4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)-
Synonyms:4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)-;DNA relaxation,ARN-21934,Inhibitor,Topoisomerase,anticancer,topoisomerase IIα,ARN 21934,inhibit,ARN21934
CAS:2230854-93-8
MF:C21H24N6
MW:360.46
EINECS:
Product Categories:
Mol File:2230854-93-8.mol
4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Structure
4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Chemical Properties
Boiling point 500.4±50.0 °C(Predicted)
density 1.230±0.06 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO : 8.33 mg/mL (23.11 mM; ultrasonic and warming and heat to 80°C)
pka9.01±0.20(Predicted)
Safety Information
MSDS Information
4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Usage And Synthesis
Biological ActivityARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research[1]. ARN-21934 display a different affinity for topoIIα and topoIIβ. ARN-21934 is more potent against the α isoform, the IC50 value for the inhibition of DNA relaxation by topoIIα is 2 μM, the value for inhibition of DNA relaxation by topoIIβ is 120 μM[1].ARN-21934 exhibits a small panel of human cancer cell lines. It against melanoma (A375 and G-361), breast (MCF7), endometrial (HeLa), lung (A549), and androgen-independent prostate (DU145) cancer cells with IC50 values of 12.6 μM, 8.1 μM, 15.8 μM, 38.2 μM, 17.1 μM, and 11.5 μM, respectively[1]. ARN-21934 (intraperitoneal injection; 10 mg/kg; single dose) reaches a maximal plasma concentration of 0.68 μg/mL after 15 min. The half-life is 149 min in circulation, still being present in plasma 360 min after injection. The compound also exhibits good clearance values (0.116 L/(min kg)). Besides, ARN-21934 is able to reach the brain, with a maximum concentration of compound at 60 min, and is still present in the brain 360 min after injection[1]
References[1]. Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.
4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Preparation Products And Raw materials
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